*  Receptor antagonist
Phenoxybenzamine is an example of an irreversible alpha blocker-it permanently binds to α adrenergic receptors, preventing ... Although they are agonists, partial agonists can act as a competitive antagonist in the presence of a full agonist, as it ... Once bound, however, antagonists inhibit the function of agonists, inverse agonists, and partial agonists. In functional ... Agonists and antagonists "compete" for the same binding site on the receptor. Once bound, an antagonist will block agonist ...
*  Arrestin beta 1
Implications for beta2-adrenergic receptor regulation". J. Biol. Chem. 274 (16): 10677-80. doi:10.1074/jbc.274.16.10677. PMID ... Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G protein- ... a beta propeller terminal domain joins an alpha zigzag linker". Cell. 95 (4): 563-73. doi:10.1016/S0092-8674(00)81623-2. PMID ... Arrestin beta 1 is a cytosolic protein and acts as a cofactor in the beta-adrenergic receptor kinase (BARK) mediated ...
*  Sepsis
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... Recombinant activated protein C (drotrecogin alpha) was originally introduced for severe sepsis (as identified by a high APACHE ...
*  Azinphos-methyl
... a cholinergic and alpha-1 adrenergic antagonist, to achieve a shorter recovery time. Treatment with a combination of different ... This phenomenon is caused by the excess of agonists (ACh) within the synapse, ultimately leading to a down-regulation of ...
*  Pramipexole
Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". The Journal ... and α2-adrenergic receptors. It has negligible affinity (>10,000 nM) for the D1, D5, 5-HT2, α1-adrenergic, β-adrenergic, H1, ... By acting as an agonist for the D2, D3, and D4 dopamine receptors, pramipexole may directly stimulate the underfunctioning ... Holman AJ, Myers RR (2005). "A randomized, double-blind, placebo-controlled trial of pramipexole, a dopamine agonist, in ...
*  ADCY9
The type 9 adenylyl cyclase is a widely distributed adenylyl cyclase, and it is stimulated by beta-adrenergic receptor ... Patke CL, Shearer WT (2000). "gp120- and TNF-alpha-induced modulation of human B cell function: proliferation, cyclic AMP ... interaction between beta-agonist and corticosteroid pathways". Hum. Mol. Genet. 14 (12): 1671-7. doi:10.1093/hmg/ddi175. PMID ... 2004). "An Ile to Met polymorphism in the catalytic domain of adenylyl cyclase type 9 confers reduced beta2-adrenergic receptor ...
*  G protein-gated ion channel
Agents that can act as agonists to this binding site can be potentially useful in the creation of drugs for the treatment of ... Studies have shown that a link exists between channels with GIRK1 subunits and the beta-adrenergic receptor pathway in breast ... Furthermore, studies have shown that G proteins, specifically the Gi alpha subunit, directly activate GIRKs which were found to ... Schubert B, VanDongen AM, Kirsch GE, Brown AM (August 1989). "Beta-adrenergic inhibition of cardiac sodium channels by dual G ...
*  GRK6
1998). "β2-Adrenergic receptor regulation by GIT1, a G protein-coupled receptor kinase-associated ADP ribosylation factor ... Zhou H, Yan F, Tai HH (2001). "Phosphorylation and desensitization of the human thromboxane receptor-alpha by G protein-coupled ... 1999). "Overexpression of wild-type and catalytically inactive forms of GRK2 and GRK6 fails to alter the agonist-induced ... 1999). "Role of G protein-coupled receptor kinases on the agonist-induced phosphorylation and internalization of the ...
*  Fluparoxan
... also exhibits no anticholinergic, antidopaminergic, alpha1-adrenergic, beta-adrenergic, muscarinic or 5-HT1-receptor ... Fluparoxan, orally prevented agonist UK-14304 induced sedation and bradycardia in a dose-related fashion in the dog. Fluparoxan ... Johnson MA, Blackwell CP, Smith J (May 1995). "Antagonism of the effects of clonidine by the alpha 2‐adrenoceptor antagonist, ... Gibbs AA, Naudts KH, Azevedo RT, David AS (April 2010). "Deletion variant of α2b-adrenergic receptor gene moderates the effect ...
*  Phenylephrine
... is a selective α1-adrenergic receptor agonist of the phenethylamine class used primarily as a decongestant, as an ... Damage may be prevented or mitigated by infiltrating the tissue with the alpha blocker phentolamine by subcutaneous injection. ... Because this medication is a sympathomimetic amine without beta-adrenergic activity, it does not increase contractility force ... Phenylephrine selectively binds to alpha receptors which cause blood vessels to constrict. Phenylephrine may cause side effects ...
*  List of MeSH codes (D12.644)
... gtp-binding protein alpha subunits, g12-g13 MeSH D12.644.360.375.100.200 --- gtp-binding protein alpha subunits, gi-go MeSH ... beta-adrenergic receptor kinase MeSH D12.644.360.200.150 --- cyclic gmp-dependent protein kinases MeSH D12.644.360.200.575 --- ... bh3 interacting domain death agonist protein MeSH D12.644.360.100 --- ca(2+)-calmodulin dependent protein kinase MeSH D12.644. ... gtp-binding protein alpha subunits, gq-g11 MeSH D12.644.360.375.100.400 --- gtp-binding protein alpha subunits, gs MeSH D12.644 ...
*  Amantadine
In 2004, it was discovered that amantadine and memantine bind to and act as agonists of the σ1 receptor (Ki = 7.44 µM and 2.60 ... It appears to be a weak NMDA receptor antagonist as well as an anticholinergic, specifically a nicotinic alpha-7 antagonist ... likely due to amantadine's dopaminergic and adrenergic activity, and to a lesser extent, its activity as an anticholinergic. ...
*  Vasodilation
... adenosine agonist, used primarily as an anti-arrhythmic alpha blockers (block the vasoconstricting effect of adrenaline) amyl ... Some sympathetic stimulation of arterioles in skeletal muscle is mediated by epinephrine acting on β-adrenergic receptors of ... Schindler, C; Dobrev, D; Grossmann, M; Francke, K; Pittrow, D; Kirch, W (January 2004). "Mechanisms of beta-adrenergic receptor ...
*  Serotonin-norepinephrine-dopamine reuptake inhibitor
Further support for the monoamine hypothesis came from monoamine depletion studies: Alpha-methyl-p-tyrosine (AMPT) is a ... Data from clinical studies have shown that DA agonists, such as bromocriptine, pramipexole and ropinirole, exhibit ... at functionally important adrenergic receptor sites in the brain. However, elation may be associated with an excess of such ... adrenergic, and dopaminergic neurotransmission. SNDRIs were developed as potential antidepressants and treatments for other ...
*  Chlorpromazine
Also associated with weight gain as a result of blockage of the adrenergic alpha 1 receptor) M1 and M2 muscarinic acetylcholine ... Posner, Lysa A.; Burns, Patrick (2009). "Chapter 13: Sedative agents: tranquilizers, alpha-2 agonists, and related agents". In ... alpha-adrenergic, and histamine receptors to clinical potency". The American Journal of Psychiatry. 137 (12): 1518-22. PMID ... and α2-adrenergic receptors (accounting for sympatholytic properties, lowering of blood pressure, reflex tachycardia, vertigo, ...
*  Treatment of Tourette syndrome
The α2-adrenergic receptor agonists (antihypertensive agents) show some efficacy in reducing tics, as well as other comorbid ... These include the alpha-2 agonists (clonidine and guanfacine), tricyclic antidepressants (desipramine and nortriptyline), and ...
*  Pindolol
... has modest beta-adrenergic agonist activity and is therefore used with caution in angina pectoris. Pindolol is a non- ... 5-HT1D alpha and 5-HT1D beta". Proc. Natl. Acad. Sci. U.S.A. 89 (8): 3630-4. doi:10.1073/pnas.89.8.3630. PMC 48922 . PMID ... selective beta blocker or β-adrenergic receptor antagonist with partial agonist activity and also possesses intrinsic ... Hoffmann C, Leitz MR, Oberdorf-Maass S, Lohse MJ, Klotz KN (2004). "Comparative pharmacology of human beta-adrenergic receptor ...
*  1-Tetralone
1977), "Adrenergic agents. 4. Substituted phenoxypropanolamine derivatives as potential β-adrenergic agonists" (in German), J. ... α-Tetralone at Sigma-Aldrich "alpha-Tetralone 529-34-0 , TCI Deutschland GmbH". www.tcichemicals.com (in German). Retrieved ... 1978), "Nondepressant β-adrenergic blocking agents. 1. Substituted 3-amino-1-(5,6,7,8-tetrahydro-1-naphthoxy)-2-propanols" (in ...
*  Cannabigerol
CBG has been found to act as a high affinity α2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and ... "Evidence that the plant cannabinoid cannabigerol is a highly potent alpha(2)-adrenoceptor agonist and moderately potent 5HT ... Evidence that the plant cannabinoid cannabigerol is a highly potent α2-adrenoceptor agonist and moderately potent 5HT1A ...
*  Indole alkaloid
Ergometrine is an agonist of α-adrenergic, 5-HT2 and partly D2 receptors. Compared with other ergot alkaloids, ergometrine has ... Dewick, p. 353 Demichel, P; Gomond, P; Roquebert, J (1982). "alpha-Adrenoceptor blocking properties of raubasine in pithed rats ... So ergotamine is a partial agonist of α-adrenergic and 5-HT2 receptors, and thus narrows blood vessels and stimulates ... Mitragynine is an agonist of the μ-opioid receptor. Harmal alkaloids are antagonists to the GABAA-receptor, and ibogaine - to ...
*  SAG (gene)
1999). "Role of the T cell receptor alpha chain in stabilizing TCR-superantigen-MHC class II complexes". Immunity. 10 (4): 473- ... Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G-protein- ... 1995). "Chromosome mapping of the human arrestin (SAG), beta-arrestin 2 (ARRB2), and beta-adrenergic receptor kinase 2 (ADRBK2 ... Yamaki K, Tsuda M, Shinohara T (1988). "The sequence of human retinal S-antigen reveals similarities with alpha-transducin". ...
*  Sodium-hydrogen exchange regulatory cofactor 2
2002). "Ca(2+)-dependent inhibition of Na+/H+ exchanger 3 (NHE3) requires an NHE3-E3KARP-alpha-actinin-4 complex for ... 2002). "The adenosine 2b receptor is recruited to the plasma membrane and associates with E3KARP and Ezrin upon agonist ... "A C-terminal motif found in the beta2-adrenergic receptor, P2Y1 receptor and cystic fibrosis transmembrane conductance ... Sodium-hydrogen exchange regulatory cofactor 2 has been shown to interact with SGK, Actinin alpha 4, Parathyroid hormone ...
*  Harris Isbell
1959b) reported that pre-treatment with scopolamine (an acetylcholine antagonist), phenoxybenzamine (an adrenergic alpha ... Clinical Aspects of Opiate Antagonists and Partial Agonists. pp 118-124 in Martin and Isbell(1978). Isbell H, Vogel VH (1949 ...
*  Serotonin
5-HT2c receptor agonist References are ignored for the functions of these receptors due to the fact they appear on the ... In macaques, alpha males have twice the level of serotonin released in the brain than subordinate males and females (as ... Additionally, it inhibits the release of norepinephrine from adrenergic nerves. Serotonin is also a growth factor for some ... Some serotonergic agonist drugs cause fibrosis anywhere in the body, particularly the syndrome of retroperitoneal fibrosis, as ...
*  Iprindole
It is presumed to act as an inhibitor or antagonist/inverse agonist of all sites. Considering the range of its therapeutic ... Iprindole also lacks significant alpha-blocking properties, and hence does not pose a risk of orthostatic hypotension. In ... Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ...
*  Olney's lesions
Drugs that work to suppress NAN include anticholinergics, benzodiazepines, barbiturates and agonists at the alpha-2 adrenergic ... Conversely, coadministration of NMDA-antagonists with alpha-2 adrenergic antagonists, like yohimbine could theoretically ...
*  Smooth muscle tissue
... adrenergic receptors), second messenger generators (adenylate cyclase, phospholipase C), G proteins (RhoA, G alpha), kinases ( ... The same preparation stimulated in normal balanced saline with an agonist such as endothelin or serotonin will generate more ... this response is mediated through alpha-1 adrenergic receptors). However, blood vessels within skeletal muscle and cardiac ... Alpha actin is also expressed as distinct genetic isoforms such as smooth muscle, cardiac muscle and skeletal muscle specific ...